Classes
DEA Class; Rx
Common Brand Names; Chloroquine phosphate
- Antimalarials;
- Antimalarials, Aminoquinoline
Description
4-aminoquinoline anti-protozoal agent
Used for treatment and prophylaxis of susceptible malaria strains and for treatment of extraintestinal amebiasis
Associated with irreversible retinal damage and life-threatening and fatal cardiomyopathy
Indications
Malaria
Prophylaxis
- Indicated for prophylaxis of malaria in geographic areas where resistance to chloroquine is not present
Treatment
- Indicated for acute attacks of malaria due to P. vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum
Contraindications
Hypersensitivity to chloroquine, 4-aminoquinolones
Psoriasis, porphyria, retinal or visual field changes
Adverse Effects
Ocular disorders: Maculopathy, macular degeneration, visual disturbances, nyctalopia, scotomatous vision with field defects of paracentral, pericentral ring types, typically temporal scotomas (eg, difficulty in reading with words tending to disappear, seeing half an object, misty vision, and fog before the eyes), reversible corneal opacities
Immune system disorders: Urticaria, anaphylactic reaction (eg, angioedema)
Ear and labyrinth disorders: Nerve type deafness, tinnitus, reduced hearing in patients with preexisting auditory damage
Musculoskeletal and connective tissue-disorders: Sensorimotor disorders, skeletal muscle myopathy or neuromyopathy, depression of tendon reflexes, abnormal nerve conduction
Gastrointestinal disorders: Hepatitis, increased liver enzymes, anorexia, nausea, vomiting, diarrhea, abdominal cramps
Skin and subcutaneous tissue disorders: Erythema multiforme, Stevens Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis, pleomorphic skin eruptions, skin and mucosal pigment changes, lichen planus-like eruptions, pruritus, drug rash with eosinophilia and systemic symptoms (DRESS syndrome), photosensitivity, hair loss
Blood and lymphatic system disorders: Pancytopenia, aplastic anemia, reversible agranulocytosis, thrombocytopenia, neutropenia, hemolytic anemia in G6PD deficient patients
Nervous system disorders: Convulsions, mild and transient headache, polyneuropathy, acute extrapyramidal disorders (eg, dystonia, dyskinesia, tongue protrusion, torticollis)
Neuropsychiatric disorders: Psychosis, delirium, anxiety, agitation, insomnia, confusion, hallucinations, personality changes, depression, suicidal behavior
Warnings
Acute extrapyramidal disorders may occur; reactions usually resolve after treatment discontinuation and/or symptomatic treatment
Not effective in most areas; CDC recommends mefloquine or atovaquone/proguanil – check CDC traveler information for specific recommendations for region
May cause hemolysis in glucose-6 phosphate dehydrogenase (G-6-PD) deficiency; blood monitoring may be needed as hemolytic anemia may occur, in particular in association with other drugs that cause hemolysis
Experimental data showed a potential risk of inducing gene mutations; there are insufficient data in humans to rule out an increased risk of cancer in patients receiving long-term treatment
Cases of cardiomyopathy resulting in cardiac failure, in some cases with fatal outcome, have been reported in patients treated during long term therapy at high doses with chloroquine; monitor for signs and symptoms of cardiomyopathy and discontinue chloroquine if cardiomyopathy develops
May cause conduction disorders (eg, bundle branch block / AV heart block) are diagnosed; if cardiotoxicity is suspected, prompt discontinuation of chloroquine may prevent life-threatening complications
Monitor knee and ankle reflexes in patients on long-term therapy to detect any evidence of muscular weakness; if weakness occurs, discontinue therapy
A number of fatalities have been reported following the accidental ingestion of chloroquine; advise to keep medication out of the reach of children because they are especially sensitive to the 4-aminoquinoline compounds
Use in patients with psoriasis may precipitate a severe attack of psoriasis; may be exacerbated condition when used in patients with porphyria; do not use in these conditions unless the benefit to the patient outweighs the potential risks
Shown to cause severe hypoglycemia including loss of consciousness that could be life-threatening in patients treated with or without antidiabetic medications; patients should be warned about risk of hypoglycemia and associated clinical signs and symptoms; patients presenting with clinical symptoms suggestive of hypoglycemia during treatment with chloroquine should have blood glucose level checked and treatment reviewed as necessary
Caution with history of auditory damage
Caution with hepatic disease, alcoholism, and coadministration with other hepatotoxic drugs
May provoke seizures in patients with history of epilepsy
Pregnancy and Lactation
Avoid use during pregnancy except in prophylaxis or treatment of malaria when benefit outweighs potential risk to fetus
Owing to the potential for serious adverse reactions in nursing infants from chloroquine, a decision should be made whether to discontinue nursing or chloroquine, taking into account the potential clinical benefit of the drug to the mother
Maximum Dosage
1,000 mg/dose (600 mg base/dose) PO for malaria up to a total of 2.5 g (1.5 g base) PO in 48 hours; 500 mg/week (300 mg base/week) PO for malaria prophylaxis; 1,000 mg/day (600 mg base/day) PO for other indications.
1,000 mg/dose (600 mg base/dose) PO for malaria up to a total of 2.5 g (1.5 g base) PO in 48 hours; 500 mg/week (300 mg base/week) PO for malaria prophylaxis; 1,000 mg/day (600 mg base/day) PO for other indications.
16.6 mg/kg/dose (10 mg base/kg/dose) [Max: 1,000 mg (600 mg base)] PO for malaria up to a total of 41.5 mg/kg (25 mg/kg base) [Max: 2.5 g (1.5 g base)] PO in 48 hours; 8.3 mg/kg/week (5 mg base/kg/week) [Max: 500 mg/week (300 mg base/week)] PO for malaria prophylaxis.
16.6 mg/kg/dose (10 mg base/kg/dose) [Max: 1,000 mg (600 mg base)] PO for malaria up to a total of 41.5 mg/kg (25 mg/kg base) [Max: 2.5 g (1.5 g base)] PO in 48 hours; 8.3 mg/kg/week (5 mg base/kg/week) [Max: 500 mg/week (300 mg base/week)] PO for malaria prophylaxis.
16.6 mg/kg/dose (10 mg base/kg/dose) PO for malaria up to a total of 41.5 mg/kg (25 mg/kg base) PO in 48 hours; 8.3 mg/kg/week (5 mg base/kg/week) PO for malaria prophylaxis.
Safety and efficacy have not been established.
How supplied
Chloroquine phosphate
tablet
- 500mg
- NOTE: Chloroquine phosphate 16.6 mg is equivalent to 10 mg chloroquine base